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Cell growth inhibitory effects of polyphenols with naphthalene skeleton against cisplatin-resistant ovarian cancer cells

机译:多酚与萘骨架对顺铂耐药卵巢癌细胞的细胞生长抑制作用

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摘要

Cisplatin often shows the drug resistance which could limit the chemotherapeutic efficacy. Thus, it is necessary to develop anticancer agents against cisplatin-resistant cancer cells. To identify pharmacophores exhibiting the cell growth inhibitory effect against cisplatin-resistant A2780/Cis ovarian cancer cells, we prepared 35 synthetic polyphenols bearing naphthalene skeleton including naphthalenyl chalcones, naphthalenyl flavones, naphthalenyl flavanones, 4,5-dihydro-1H-pyrazol-3-yl)naphthalen-2-ols, naphthalen-1-yl-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamides, and 4,5-dihydro-1H-pyrazol-3-yl)naphthalen-1-ol. The correlation between their inhibitory effects and structural properties was evaluated using hologram quantitative structure activity relationship and comparative molecular field analysis. The pharmacophores derived here can lead us to design new polyphenols against the growth of cisplatin-resistant cells.
机译:顺铂通常显示可能限制化学治疗效果的耐药性。 因此,有必要对抗顺铂抗性癌细胞进行抗癌剂。 为了鉴定表现出对抗顺铂A2780 /顺式卵巢癌细胞的细胞生长抑制作用的药物,我们制备了35种合成多酚亚萘骨架,包括萘基Chalcones,萘基黄酮,萘基黄酮,4,5-二氢-1H-吡唑-3- Y1)萘-2-醇,萘-1-基 - 苯基-4,5-二氢-1H-吡唑-1-碳磷酸,4,5-二氢-1H-吡唑-3-基)萘-1 -ol。 通过全息图定量结构活性关系和比较分子场分析评估其抑制作用与结构性能之间的相关性。 衍生的药物细胞可以引导我们设计新的多酚免受顺铂抗性细胞的生长。

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